Effect of cationic surfactant on transport of surface-active and non-surface-active model drugs and emulsion...

A study was carried out to determine the effect of excess surfactant on transport kinetics in emulsions, using surface-active (phenobarbital, barbital) and non-surface-active (phenylazoaniline, benzocaine) model drugs (pH 7.0). Mineral oil was chosen as the oil phase, and the ionic surfactant cetyltrimethylammonium bromide (CTAB) was chosen as the emulsifier. The effect of nonionic surfactant Brij 97 on transport kinetics of these model drugs were determined by authors elsewhere. Model drug transport in the triphasic systems was investigated using side-by-side diffusion cells mounted with hydrophilic dialysis membranes (molecular weight cutoffs 1 kD and 50 kD) and a novel bulk equilibrium reverse dialysis bag technique. Emulsion stability was determined by droplet size analysis as a function of time, temperature, and the presence of model drugs using photon correlation spectroscopy. Mineral oil/water partition coefficients and aqueous solubilities were determined in the presence of surfactant. The droplet size of the CTAB-stabilized emulsion system is bigger than that of the Brij 97-stabilized system because of the relatively less dense interfacial packing of the cationic surfactant. CTAB forms a complex with the model drugs because of ionic interaction between CTAB and the aromatic and azo groups of the model drugs. This complexation is expected to increase emulsion stability and affect model drug transport kinetics. The transport rates of model drugs in emulsions increased with increases in CTAB micellar concentrations up to 0.5% w/v and then decreased at higher surfactant concentrations. Total transport rates of phenobarbital and barbital were faster than those of phenylazoaniline and benzocaine. Excess surfactant affected the transport rates of the model drugs in the emulsions depending on drug surface activity and lipophilicity. The transport profiles of the model drugs appeared to be governed by model drug oil/water partition coefficient values and by micellar shape changes at higher surfactant concentrations.